产品货号：
M04757
中文名称：
CRTh2(DP2;GPR44)抑制剂(AZD1981)
英文名称：
AZD1981
产品规格：
1mL(10mM)|5mg|10mg|50mg|100mg
发货周期：
1～3天
产品价格：
询价
AZD1981是CRTh2(DP2;GPR44)高效选择性抑制剂。
注：本品仅可用于科研实验，严禁用于临床医疗及其他用途！
CAS号：802904-66-1
纯度：99.52%
分子式：C19H17ClN2O3S
分子量：388.87
溶解性：DMSO≥31mg/mL(79.72mM)
结构式：
保存：-20℃，有效期2年，溶入溶剂后-20℃请尽量在一个月内使用。
AZD1981 is a potent and selective CRTh2 antagonist;displaces radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4).IC50 value:Target:GPR44 antagonist in vitro:AZD1981 produced a concentration-dependent displacement of the [3H]PGD2-specific binding with a mean pIC50 of 8.4 ± 0.1 (n = 25,geometric mean IC50 of 4 nM).AZD1981 had no significant affinity towards recombinant human DP1 receptors with only a mean 27% (range 14～50%;n = 4) displacement of [3H]PGD2-specific binding observed at the highest concentration tested (10μM).Compared with the binding potency for DP2,AZD1981 showed 10-fold selectivity over rat aldose reductase and 1700-fold selectivity over rat steroid 5α-reductase.In eosinophils,a single concentration of 1μM,AZD1981 caused a large (20-fold) rightward parallel shift in the 15R-methyl PGD2 E/[A] curve with no evidence of a decrease in the maximal response.The effect of AZD1981 was therefore investigated using a single sub-maximal concentration of agonist (1μM).AZD1981 produced a concentration-dependent inhibition of eosinophil migration with a pIC50 value of 7.6 ± 0.1 (n = 4).in vivo:Using the previously described guinea pig hind limb model,10 nM AZD1981 significantly inhibited DK-PGD2-induced eosinophil mobilization by approximately 50%,and the response was completely inhibited with 100 nM AZD1981.in vivo:AZD1981 exhibited good cross-species binding activity against mouse,rat,guinea pig,rabbit and dog DP2.Evaluation in mouse,rat or rabbit cell systems was not possible as they did not respond to DP2 agonists.Agonist responses were seen in guinea pig and dog,and AZD1981 blocked DP2 -mediated eosinophil shape change.Such responses were more robust in the guinea pig,where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow.There was no beneficial clinical effect of AZD1981,at a dose of 1000mg twice daily for 4 weeks,in patients with moderate to severe COPD.AZD1981 was well tolerated and no safety concerns were identified.
相关搜索：CRTh2(DP2;GPR44)抑制剂(AZD1981)，802904-66-1
注：本品仅可用于科研实验，严禁用于临床医疗及其他用途！
CAS号：802904-66-1
纯度：99.52%
分子式：C19H17ClN2O3S
分子量：388.87
溶解性：DMSO≥31mg/mL(79.72mM)
结构式：
保存：-20℃，有效期2年，溶入溶剂后-20℃请尽量在一个月内使用。
AZD1981 is a potent and selective CRTh2 antagonist;displaces radio-labelled PGD2 from human recombinant DP2 with high potency (pIC50 = 8.4).IC50 value:Target:GPR44 antagonist in vitro:AZD1981 produced a concentration-dependent displacement of the [3H]PGD2-specific binding with a mean pIC50 of 8.4 ± 0.1 (n = 25,geometric mean IC50 of 4 nM).AZD1981 had no significant affinity towards recombinant human DP1 receptors with only a mean 27% (range 14～50%;n = 4) displacement of [3H]PGD2-specific binding observed at the highest concentration tested (10μM).Compared with the binding potency for DP2,AZD1981 showed 10-fold selectivity over rat aldose reductase and 1700-fold selectivity over rat steroid 5α-reductase.In eosinophils,a single concentration of 1μM,AZD1981 caused a large (20-fold) rightward parallel shift in the 15R-methyl PGD2 E/[A] curve with no evidence of a decrease in the maximal response.The effect of AZD1981 was therefore investigated using a single sub-maximal concentration of agonist (1μM).AZD1981 produced a concentration-dependent inhibition of eosinophil migration with a pIC50 value of 7.6 ± 0.1 (n = 4).in vivo:Using the previously described guinea pig hind limb model,10 nM AZD1981 significantly inhibited DK-PGD2-induced eosinophil mobilization by approximately 50%,and the response was completely inhibited with 100 nM AZD1981.in vivo:AZD1981 exhibited good cross-species binding activity against mouse,rat,guinea pig,rabbit and dog DP2.Evaluation in mouse,rat or rabbit cell systems was not possible as they did not respond to DP2 agonists.Agonist responses were seen in guinea pig and dog,and AZD1981 blocked DP2 -mediated eosinophil shape change.Such responses were more robust in the guinea pig,where AZD1981 also blocked DP2 -dependent eosinophil emigration from bone marrow.There was no beneficial clinical effect of AZD1981,at a dose of 1000mg twice daily for 4 weeks,in patients with moderate to severe COPD.AZD1981 was well tolerated and no safety concerns were identified.
相关搜索：CRTh2(DP2;GPR44)抑制剂(AZD1981)，802904-66-1